Enzyme Modulators

Inhibitor of ataxia telangiectasia mutated (ATM) kinase and AKT kinase with anti-cancer activity. ATM is a nuclear protein kinase and a signal transducer sensing DNA damage as well as controlling double strand DNA break (DSB) repair. It is a radiotherapy and chemotherapy sensitizer, especially in tumors sensitive to DNA alkylating agents (such as temozolomide). Moreover, KU 55933 inhibits phosphorylation of cytoplasmic AKT kinase, downregulates synthesis of cyclin D1 and induces cell cycle arrest in G1 phase.

Substrate peptide for protein tyrosine phosphatase 1B (PTP1B)- an ubiquitously expressed non-receptor tyrosine phosphatase. PTP1B negatively regulates signalling pathways controlling metabolic homeostasis, cell proliferation and immunity (such as leptin and insulin receptor signalling), making PTP1B an interesting target for type 2 diabetes mellitus (T2DM) and obesity treatment. PTP1B also has important leptin-independent metabolic effects, playing a critical role in the regulation of inflammation, cell proliferation, differentiation and invasion. Therefore PTP1B is also interesting as a therapeutic target for inflammatory and autoimmune diseases and cancer.-For application data please see: Figure 2 supplement 1C.

Inhibitor of COX-1 and COX-2 cyclooxygenases

Inhibitor of protein kinase CK2

Inhibits RNAPII-mediated trasncription; immunosuppressant; anti-inflammatory

A potent selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE-5), thereby reducing the degradation rate of cGMP. Sildenafil is used to treat erectile dysfunction and pulmonary arterial hypertension. Sildenafil citrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Metformin is a widely used anti-hyperglycemic (anti-diabetic) agent for the treatment of type 2 diabetes mellitus. This is due to it decreasing blood glucose by decreasing hepatic glucose product by activation of the AMP-activated protein kinase AMPK. Studies have also demonstrated Metformin to have anti-cancer activity, attributed to several mechanisms such as inhibition of mammalian target of rapamycin (mTOR), cancer stem cells and inflammation. Metformin HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells

DARKtide is a substrate peptide for death-associated protein kinase (DAPK) for use in kinases assays. DAPK is involved in several cellular pathways including: apoptosis, tumour suppression, stress response, anti-viral immunity and IL-1-associated inflammatory diseases. In C. elegans DAPK-1 regulates epidermal morphogenesis, innate immunity and wound repair.

Proteosome inhibitor; antineoplastic

Loxoprofen is a non-steroidal anti-inflammatory drug that belongs to the group of propionic acid derivatives. It can be used for the treatment of pain and inflammation associated with osteoarthritis, rheumatoid arthritis and other musculoskeletal disorders. Its therapeutic effects are attributed to inhibition of cyclooxygenases 1 and 2 (COX-1 and COX-2) enzymes. Loxoprofen sodium is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of CSF1R receptor

Inhibitor of Janus kinase JAK-1

GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.

Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values of 8 nM and 28 nM, respectively. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and potentiates senescence in vitro and in zebrafish model of hepatocellular carcinoma. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.

Potent inhibitor of dual specificity tyrosine-phosphorylation-regulated kinase 3 (DYRK3) with IC50 value of 0.7 nM. Elevates hemoglobin and platelet levels in anemic mice.

Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties. Tacrolimus is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Diflunisal is a nonsteroidal anti-inflammatory drug (NSAID), which is a synthetic derivative of salicylic acid. It is primarily sourced through chemical synthesis rather than extraction from natural elements. Diflunisal functions by inhibiting the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which play a crucial role in the biosynthesis of prostaglandins. This inhibition results in reduced production of prostaglandins, compounds involved in inflammation and pain signaling pathways. The primary applications of Diflunisal are in the management of mild to moderate pain and inflammatory conditions. It is often utilized in the treatment of conditions such as osteoarthritis and rheumatoid arthritis. Its analgesic properties make it effective for addressing musculoskeletal pain and postoperative discomfort. Due to its mechanism of action, Diflunisal provides anti-inflammatory, analgesic, and antipyretic effects, which can be beneficial in clinical settings where inflammation and pain management are critical. However, its usage must be monitored due to potential side effects associated with NSAID use, such as gastrointestinal irritation and cardiovascular risks. Scientists continue to explore various applications and improve the therapeutic index of Diflunisal through modified formulations and targeted delivery approaches.

Inhibitor of chymotrypsin

Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic